乏氧显像剂1-H-1-(3-~(18)F-2-羟基丙基)-2-硝基咪唑的自动化合成

Automated Synthesis of ~(18)F-Labelled Fluoromisonidazole as Hypoxia Imaging Agent

摘要: 为了制备1 H 1 (3 18F 2 羟基丙基) 2 18F 硝基咪唑(18 F FMISO),采用“一锅法”和 Tracerlab FXF N自动化合成装置,以1 (2’ 硝基 1’ 咪唑基) 2 O 四氢吡喃基 3 O 甲苯磺酰基丙二醇为原料,经亲核氟化、水解两步反应制备18F FMISO注射液。总合成时间小于60 min,放化产率和放化纯度分别大于 60%和 99%。采用“一锅法”自动化合成18F FMISO,操作简便,能满足科研和临床正电子发射断层显像的需要。

Abstract: H-1-(3-~(18)F-fluoro-2-hydroxylpropyl)-2-nitroimidazole(~(18)F-FMISO) is synthesized by “one pot” method at Tracerlab FX_(F-N) system. By using 1-(2’-nitro-1’-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonyl-propanediol as the precursor, ~(18)F-FMISO is obtained via two-step reactions, including the nucleophilic fluoration of the precursor to yield an intermediate 1-(2’-nitro-1’-imidazolyl)-2-O-tetrahydropyranyl)-3-~(18)F-fluoropropanol, and the acidic hydrolysis of the intermediate. The procedure is guite simple and can be completed within 60 min. The radiochemical yield and radiochemical purity are higher than 60% and 99%, respectively. Toxicological assays indicate that the final product is bacteria-free and non-toxic, and meets the requirements for radiopharmacy. It can be used in clinical and scientific research.